JPH1087457A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral cavity, capable of stably keeping germicidal activity of a cationic germicide and exhibiting foaming properties having high foaming power and high foam retaining property by compounding a nonionic surfactant with a carboxylic acid type ampholytic surfactant at a specific ratio. SOLUTION: This composition contains (A) 0.01-5wt.% cationic germicide, (B) 1-15wt.% nonionic surfactant (preferably a highly hydrophilic nonionic surfactant having >=10 HLB value, especially preferably polyoxyethylene polyoxypropylene copolymer) and (C) 0.1-3wt.% carboxylic acid type ampholytic surfactant (preferably an alkylbetaine type ampholytic surfactant). The composition is used by packing the composition into a foamer container having a porous membrane and discharging the composition so as to become foamy state from the container. The composition is effective in suppressing plaque in oral cavity and preventing periodontal diseases and dental caries.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition which is discharged as a foam by being mixed with air and passing through a porous membrane. The present invention relates to an oral composition which is effective in suppressing plaque formation by being maintained and preventing periodontal disease and dental caries.

[0002]

2. Description of the Related Art Conventional dentifrices on the market include:
Kneaded or liquid dosage forms are mainly used.
However, kneaded ones take time to disperse in the mouth, and liquid ones have excellent dispersibility and penetrability in the mouth but have fluidity and can be placed on the toothbrush and placed on the mouth. It has problems such as difficulty in carrying.

[0003] In order to solve such a problem, a foamy dosage form is conceivable.
927, JP-B-62-15524, JP-B-62-1
No. 5525, JP-B 8-25859, JP-A-63-2
In 2011 and JP-A-63-233908, a method has been proposed in which a propellant is mixed with an oral composition, filled into an aerosol container, and foamed. However, the propellant is not preferable because it not only has a problem in safety when applied in the oral cavity, but also has a bad influence on the environment.

[0004] In order to form a foam without using a propellant, there is a method in which the composition is mixed with air and passed through a porous membrane to fill a former container having a structure in which the composition is discharged as a foam. Numerous patents have been disclosed in the field of "skin cleansing" for compositions filled in such containers. Other techniques disclosed as general detergents include “foaming detergent” in JP-A-5-132700 and JP-A-8-132700.
92064 and JP-A-8-143899, "Aqueous liquid detergent"; JP-A-8-131809, "Composition for non-gas former"; JP-A-8-143854, "Chemical agent applied to pump-type former" Compositions ".

However, among these, Japanese Patent Application Laid-Open No. 8-143
No. 854 discloses a surfactant concentration of 0.01 to
As low as 1.0% by weight or less, the compounding amount of the surfactant used in the present invention is not suitable because of insufficient foaming properties, and has been proposed as a foaming agent as disclosed in JP-A-8-92064. Many of the present surfactants are bitter or irritating to the oral mucosa and are not suitable for oral use.

On the other hand, cationic bactericides are useful for plaque control due to their high bactericidal properties and retention in the oral cavity. However, in order to stably incorporate the cationic bactericides, it is necessary to carefully consider surfactants that have a particularly large effect. It is best to choose.

In order to fill this composition into a foamer container having a porous membrane and discharge it as a foam, it is necessary to incorporate a surfactant having excellent foaming properties and foam retention properties. Among the surfactants which are considered to be suitable for the stable formulation of the cationic bactericide, nonionic surfactants generally have poor foaming properties and poor foam retention. In addition, many amphoteric surfactants have good foaming properties and foam retention properties, but generally have a poor taste, and it is difficult to mix them in an amount sufficient to obtain satisfactory foam properties. In addition, cationic surfactants are highly irritating to mucous membranes, and it is not preferable to mix them in large amounts.

[0008]

SUMMARY OF THE INVENTION An object of the present invention is to provide a composition filled in a former container which is discharged as a foam by being mixed with air and passing through a porous membrane.
It is an object of the present invention to provide a composition for an oral cavity that maintains the bactericidal activity of a cationic bactericide stably, has good physical properties of foam to be discharged, and is excellent in usability.

[0009]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to solve such problems, and as a result, a nonionic surfactant and a carboxylic acid-type amphoteric surfactant are mixed at a specific ratio. By doing so, it has been found that the bactericidal activity of the cationic bactericide can be stably maintained and foam properties having high foaming properties and foam retention properties can be obtained, and the present invention has been completed.

That is, the present invention relates to (a) 0.01 to 5% by weight of a cationic bactericide, (b) 1 to 15% by weight of a nonionic surfactant, and (c) a carboxylic acid type amphoteric surfactant. A liquid composition containing 0.1 to 3% by weight is filled in a foamer container having a porous membrane, and when the liquid composition is discharged from the container, the composition becomes a foam. Things. According to the present invention, since the bactericidal activity of the cationic bactericide is sufficiently exhibited, it is effective in preventing periodontal disease and dental caries, and is discharged as a foam having good foam physical properties, thereby giving a feeling of use. An excellent oral composition can be provided.

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION The cationic bactericide used in the present invention includes a bisbiguanide compound or a quaternary ammonium salt, and specifically, chlorhexidine gluconate, chlorhexidine hydrochloride, cetylpyridinium chloride, benzethonium chloride. And the like. These cationic fungicides can be used alone or in combination of two or more kinds. The compounding amount is 0.01 to 5% by weight, particularly 0.01 to 0. 0% by weight based on the whole oral composition.
5% by weight is preferred.

The nonionic surfactants used in the present invention include polyoxyethylene polyoxypropylene copolymers, alkyl polyoxyethylene ethers, fatty acid alkanolamides, fatty acid sucrose esters, polyoxyethylene castor oil and Hydrogenated castor oil, polyoxyethylene sorbitan fatty acid esters, fatty acid polyglycerin esters, etc., among which HLB
A highly hydrophilic polymer having a value of 10 or more is preferable, and a polyoxyethylene polyoxypropylene copolymer is particularly preferable.
The polyoxyethylene polyoxypropylene copolymer is specifically manufactured by Plur of BASF Corporation, USA.
onic P-65, Pluronic F-88,
Pluronic P-105 and the like. These nonionic surfactants can be compounded alone or in combination of two or more, and the compounding amount is 1 to 15% by weight, particularly 2 to 10% by weight based on the whole oral composition.
Is preferred. If the amount is less than 1% by weight, the foamability is low, and the foam is not discharged as a foam having good physical properties. If it exceeds 15% by weight, the cationic bactericide may be inactivated and the bactericidal activity may not be sufficiently exhibited.

Examples of the carboxylic acid type amphoteric surfactant used in the present invention include betaine type, imidazolium type, imidazolium betaine type, amino acid type and amine oxide type. Among them, coconut oil fatty acid alkylamide betaine, lauryl Alkyl betaine-type amphoteric surfactants such as betaine dimethylaminoacetate are preferred. These carboxylic acid-type amphoteric surfactants can be used alone or in combination of two or more, and the amount thereof is 0.1 to 3% by weight, especially 0.2 to 3% by weight based on the whole oral composition. ~ 1.
5% by weight is preferred. When the amount is less than 0.1% by weight, the discharged foam has poor foam retention, causing defoaming and water separation. On the other hand, if it exceeds 3% by weight, bitterness is exhibited, which is not preferred.

The oral composition of the present invention contains, in addition to the above-mentioned nonionic surfactant and carboxylic acid type amphoteric surfactant, other surfactants usually used for oral compositions. It can be blended within a range that does not impair the effects of the invention.

The oral composition of the present invention contains, in addition to the cationic bactericide and the surfactant, components usually used in the oral composition, such as wetting agents, monohydric alcohols, thickeners, and fragrances. , Sweeteners, pH adjusters, preservatives, pigments, etc.
It can be appropriately compounded within a range that does not impair the effects of the present invention. However, since the composition for oral cavity of the present invention is used after being filled in a former container having a porous film, a water-insoluble powder such as an abrasive which causes clogging of the porous film is not blended.

Examples of the humectant include glycerin, sorbitol, polyethylene glycol, propylene glycol, ethylene glycol, 1,3-butylene glycol, polypropylene ghoul, xylit, and maltite.
Polyhydric alcohols such as lactit can be used alone or in combination of two or more. The compounding amount is usually 3 to 20% by weight based on the whole composition.

The monohydric alcohol includes, for example, methanol, ethanol, propyl alcohol, isopropyl alcohol and the like, and ethanol is particularly preferable. These monohydric alcohols can be used alone or in combination of two or more, and the amount is usually 1 to 15% by weight based on the whole composition.

Examples of the thickener include cellulose derivatives such as carrageenan and carboxymethyl cellulose; alkali metal alginate such as sodium alginate; gums such as xanthan gum, tragacanth gum and gum arabic; and synthetic thickeners such as polyvinyl alcohol and sodium polyacrylate. Binders, silica gel, aluminum silica gel, inorganic binders such as veegum and the like, and these can be used alone or in combination of two or more so that the viscosity at 25 ° C. of the composition becomes 100 cps or less. . If it exceeds 100 cps, the composition becomes difficult to pass through the porous membrane, and bubbles may not be discharged.
The compounding amount of these thickeners is usually 0.01 to 5% by weight based on the total amount of the composition.

Examples of the flavoring agent include menthol, carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronell, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineole , Linalool, ethyl linalool, crocodile, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil,
Winter green oil, clove oil, eucalyptus oil and the like can be mentioned, and these can be used alone or in combination of two or more.

Examples of the sweetener include saccharin sodium, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatyl phenylalanyl methyl ester, ρ-methoxycinnamic aldehyde and the like. These can be used alone or in combination of two or more. The compounding amount is usually 0.01 to 1% by weight, preferably 0.05 to 0.5% by weight based on the whole composition.

Examples of the pH adjuster include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid,
Glycerophosphoric acid, acetic acid, nitric acid, or a chemically possible salt thereof, sodium hydroxide, and the like, and these may be used alone or in combination of two or more such that the pH of the composition is in the range of 5 to 9. Can be blended. The compounding amount is usually 0.01 to 2% by weight based on the whole composition.

Furthermore, the oral composition of the present invention contains non-cationic ingredients such as vitamin Es such as dL-α-tocopherol acetate, tocopherol succinate or tocopherol nicotinate, and non-active ingredients such as triclosan. Ionic fungicides, amphoteric fungicides such as dodecyl diaminoethyl glycine, enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (Litech enzyme), sodium monofluorophosphate, potassium monofluorophosphate, etc. Fluorides such as alkali metal monofluorophosphate, sodium fluoride, stannous fluoride, tranexamic acid, epsilon aminocaproic acid, aluminum chlorohydroxyl allantoin, dihydrocholesterol, glycyrrhizin salts, Rurechin acid, glycerophosphate, chlorophyll, sodium chloride, Karopeputaido, a water-soluble inorganic phosphoric acid compounds may be blended singly or in combination of two or more.

The composition for oral cavity of the present invention can be produced by mixing these components according to a conventional method, and the obtained composition is filled in a former container having a porous membrane.

The former container for filling the oral composition of the present invention is a foamer which is discharged as a foam by mixing the composition with air by pressing and pressing the container and passing the mixture through a porous membrane. Either may be used. For example, the pressurizing method includes a squeeze former of a type in which the body of a soft container is pressed with a finger, and a pump former of a type in which the head of a cap provided with a pump mechanism is pressed with a finger. For example, in the case of
Containers described in JP-A-215352 and JP-A-7-215353 can be used.

[0025]

EXAMPLES Next, the present invention will be described in more detail with reference to Test Examples and Examples, but the present invention is not limited thereto. All of the compounding amounts in the examples mean% by weight.

Test Example Sample Preparation Method The sample solution was prepared by adding a monohydric alcohol, a polyhydric alcohol, a flavor, a sweetener, and a common component in addition to the components of the cationic bactericide and the surfactant shown in Table 1. A certain amount of each adjusting agent was blended and prepared, and subjected to the following tests.

Test Example 1: Bactericidal activity test 5 ml of each sample solution had a Streptococcus mutans concentration of 108 to 109 CFU / ml.
Us mutans) 0.1 ml of the bacterial suspension was added, and a sterilization reaction was carried out at 37 ° C. for 5 minutes in a hot water bath.
% And 0.7% Resin
Agar (TSA) coated on a flat plate under anaerobic conditions (N2 /
(H2 / CO2 = 85/10/5) at 37 ° C for 2 days, and the minimum bactericidal concentration (%) (hereinafter referred to as MBC) was measured. As a standard, a 0.1% aqueous solution of cetylpyridinium chloride or a 0.05% aqueous solution of chlorhexidine gluconate was used. The standard MBC was 0.0005% cetylpyridinium chloride and 0.05% chlorhexidine gluconate. The evaluation was performed according to the following criteria. Table 1 shows the results.・ ・ ・: MBC of test sample is equivalent to standard MBC,
Or less ×: MBC of test sample is larger than standard MBC

Test Example 2: Measurement of physical properties of foam Evaluation of foaming property Each component described in Table 1 was prepared by stirring and mixing according to a conventional method, and the mixture was filled in a pump former having a porous membrane of 200 mesh, and a certain amount of the composition and air were mixed. When the foam was discharged into a cylindrical container having a diameter of 5 cm, the height H of the top of the foam immediately after the discharge was measured. The evaluation was performed according to the following criteria. Table 1 shows the results. ○ ・ ・ ・ H> 5cm × ・ ・ ・ H ≦ 5cm Evaluation of foam retention property H was measured in the same manner as described above, and the height h of the top of the foam after standing for 5 minutes was measured. The evaluation was performed according to the following criteria. Table 1 shows the results. ○ ・ ・ ・ h> 4.5cm × ・ ・ ・ H ≦ 4.5cm or water separated

[0029]

[Table 1]

As is clear from the results in Table 1, when an anionic surfactant is used, the foam properties are good, but the bactericidal power of the cationic bactericide is inactivated. In addition, even when a nonionic surfactant and an amphoteric surfactant are used in combination,
If the amount of the nonionic surfactant is less than 1%, the foaming property is low, and if it exceeds 15%, the bactericidal activity of the cationic bactericide is inactivated. Further, the amount of the amphoteric surfactant used in combination is 0.1.
If it is less than 1%, the foam retention is poor and water separation occurs.

Example 4 The following components were prepared according to a conventional method, and filled in a pump-type former container having a porous membrane of 150 mesh. Component Content (%) Chlorhexidine hydrochloride 0.02 Polyoxyethylene (38) Polyoxypropylene (30) Glycol 12.0 Coconut oil fatty acid amidopropyl betaine 1.0 Glycerin 15.0 Sorbitol 2.0 Ethanol 5.0 Fragrance 1.0 Saccharin 0.1 Sodium hydrogen phosphate 0.1 Sodium fluoride 0.3 Purified water Balance Total 100.0

Example 5 The following components were prepared according to a conventional method, and filled in a squeeze-type former container having a 200-mesh porous membrane. Ingredient Content (%) Cetylpyridinium chloride 0.05 Polyoxyethylene (4.2) lauryl ether 10.0 Lauryl dimethylaminoacetic acid betaine 0.5 Glycerin 10.0 Propylene glycol 5.0 Ethanol 10.0 Perfume 8 Stevia extract 0.2 Trisodium citrate 0.1 Citric anhydride 0.05 dL-α-tocopherol acetate 0.02 Purified water Balance Total 100.0

Example 6 The following components were prepared according to a conventional method, and filled in a squeeze-type former container having a 200-mesh porous membrane. Component Blended amount (%) Benzalkonium chloride 0.05 Polyoxyethylene (104) Polyoxypropylene (35) Glycol 7.0 2-Alkyl-N-carboxymethyl N-hydroxyethyl imidazolium betaine 0.5 Glycerin 18 2.0 Ethanol 2.0 Sodium carboxymethylcellulose 0.1 Fragrance 0.5 Saccharin 0.25 Sodium monofluorophosphate 0.7 Allantoin 0.05 Purified water Balance Total 100.0 Oral compositions of Examples 4 to 6 All had good bactericidal activity and foam properties.

[0034]

According to the present invention, it is possible to provide a composition for the oral cavity which maintains the bactericidal activity of the cationic bactericide stably, has good physical properties of the foam to be discharged, and is excellent in usability.

Claims (4)

[Claims] (1) 0.01 to 5% by weight of a cationic bactericide, (b) 1 to 15% by weight of a nonionic surfactant, and (c) 0.1 to 5% by weight of a carboxylic acid type amphoteric surfactant. An oral composition, wherein a liquid composition containing 3% by weight is filled in a former container having a porous membrane, and when it is discharged from this container, it forms a foam. 2. The oral composition according to claim 1, wherein the nonionic surfactant has an HLB value of 10 or more. 3. The oral composition according to claim 1, wherein the nonionic surfactant is a polyoxyethylene polyoxypropylene copolymer. 4. The oral composition according to claim 1, wherein the carboxylic acid type amphoteric surfactant is a betaine type amphoteric surfactant.